Substituted benzoic acids, inhibitors of phospholipases A.sub.2
US5374772A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Oct 22, 1993 |
| Grant date | Dec 20, 1994 |
| Priority date | — |
| Expiry date | Oct 22, 2013 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07C69/92
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
The invention relates to compounds of the formula ##STR1## R is hydrogen, lower alkyl, --(CH.sub.2).sub.2 N(R.sub.3).sub.2 or --CH.sub.2 OOCR.sub.3 wherein R.sub.3 is lower alkyl; PA1 R.sub.1 is CH.sub.3 (CH.sub.2).sub.n --, wherein n is 0-17, or R.sub.4 (CH.sub.2).sub.p --, wherein p is 2-18 and R.sub.4 is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl; PA1 R.sub.2 is R.sub.4 (CH.sub.2).sub.p --, 1-adamantyl--CO-- or diphenylmethyl--CO--, and, when R is hydrogen, pharmaceutically acceptable salts with bases. The compounds of formula I are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.